公开(公告)号：US20130225572A1

公开(公告)日：2013-08-29

申请号：US13617683

申请日：2012-09-14

申请人： Makoto OKADA ,  Shuichiro SATO ,  Kenji KAWADE ,  Kotaro GOTANDA ,  Atsushi SHINBO ,  Youichi NAKANO ,  Hideo KOBAYASHI

发明人： Makoto OKADA ,  Shuichiro SATO ,  Kenji KAWADE ,  Kotaro GOTANDA ,  Atsushi SHINBO ,  Youichi NAKANO ,  Hideo KOBAYASHI

IPC分类号： C07D487/14 ,  C07D487/04

CPC分类号： C07D487/04 ,  C07D487/14

摘要： The invention discloses quinoxaline derivatives or salts thereof having PDE9-inhibiting activity and being useful as treating agent of dysuria and the like, which are represented by the formula (I) in the formula, R1 and R2 each independently stands for hydrogen, halogen, alkyl, alkoxy, acyl, amino and the like, R3 stands for alkyl, aryl, saturated carbocyclic group, saturated heterocyclic group, acyl and the like, R4 stands for hydrogen, hydroxy, alkyl or amino, R5 and R8 each independently stands for hydrogen, halogen, alkyl, alkenyl, alkoxy, cyano or nitro, R6 and R7 each independently stands for hydrogen, halogen, alkyl, alkenyl, alkynyl, alkoxy, cyano, amino, carbocyclic group, heterocyclic group, COR9 or SO2R9, R9 stands for hydrogen, hydroxy, alkyl, amino, pyrrolidin-1-yl, piperidin-1-yl, pyperazin-1-yl or the like, X stands for S or O, and A1, A2 and A3 each independently stands for N or C.

摘要翻译： 本发明公开了具有PDE9抑制活性的喹喔啉衍生物或其盐，可用作式（I）所示的排尿困难等的治疗剂，R 1和R 2各自独立地表示氢，卤素，烷基 烷氧基，酰基，氨基等，R3代表烷基，芳基，饱和碳环基，饱和杂环基，酰基等，R4代表氢，羟基，烷基或氨基，R5和R8各自独立代表氢， 卤素，烷基，烯基，烷氧基，氰基或硝基，R6和R7各自独立地代表氢，卤素，烷基，烯基，炔基，烷氧基，氰基，氨基，碳环基，杂环基，COR9或SO2R9，R9代表氢， 羟基，烷基，氨基，吡咯烷-1-基，哌啶-1-基，哒嗪-1-基等，X表示S或O，并且，A1，A2和A3各自独立地表示N或C.

公开(公告)号：US08299080B2

公开(公告)日：2012-10-30

申请号：US12448212

申请日：2007-12-12

申请人： Makoto Okada ,  Shuichiro Sato ,  Kenji Kawade ,  Kotaro Gotanda ,  Atsushi Shinbo ,  Youichi Nakano ,  Hideo Kobayashi

发明人： Makoto Okada ,  Shuichiro Sato ,  Kenji Kawade ,  Kotaro Gotanda ,  Atsushi Shinbo ,  Youichi Nakano ,  Hideo Kobayashi

IPC分类号： A61K31/495

CPC分类号： C07D487/04 ,  C07D487/14

摘要： The invention discloses quinoxaline derivatives or salts thereof having PDE9-inhibiting activity and being useful as treating agent of dysuria and the like, which are represented by the formula (I) in the formula, R1 and R2 each independently stands for hydrogen, halogen, alkyl, alkoxy, acyl, amino and the like, R3 stands for alkyl, aryl, saturated carbocyclic group, saturated heterocyclic group, acyl and the like, R4 stands for hydrogen, hydroxy, alkyl or amino, R5 and R8 each independently stands for hydrogen, halogen, alkyl, alkenyl, alkoxy, cyano or nitro, R6 and R7 each independently stands for hydrogen, halogen, alkyl, alkenyl, alkynyl, alkoxy, cyano, amino, carbocyclic group, heterocyclic group, COR9 or SO2R9, R9 stands for hydrogen, hydroxy, alkyl, amino, pyrrolidin-1-yl, piperidin-1-yl, pyperazin-1-yl or the like, X stands for S or O, and A1, A2 and A3 each independently stands for N or C.

摘要翻译： 本发明公开了具有PDE9抑制活性的喹喔啉衍生物或其盐，可用作式（I）所示的排尿困难等的治疗剂，R 1和R 2各自独立地表示氢，卤素，烷基 烷氧基，酰基，氨基等，R3代表烷基，芳基，饱和碳环基，饱和杂环基，酰基等，R4代表氢，羟基，烷基或氨基，R5和R8各自独立代表氢， 卤素，烷基，烯基，烷氧基，氰基或硝基，R6和R7各自独立地代表氢，卤素，烷基，烯基，炔基，烷氧基，氰基，氨基，碳环基，杂环基，COR9或SO2R9，R9代表氢， 羟基，烷基，氨基，吡咯烷-1-基，哌啶-1-基，哒嗪-1-基等，X表示S或O，并且，A1，A2和A3各自独立地表示N或C.

公开(公告)号：US20100048556A1

公开(公告)日：2010-02-25

申请号：US12448212

申请日：2007-12-12

申请人： Makoto Okada ,  Shuichiro Sato ,  Kenji Kawade ,  Kotaro Gotanda ,  Atsushi Shinbo ,  Youichi Nakano ,  Hideo Kobayashi

发明人： Makoto Okada ,  Shuichiro Sato ,  Kenji Kawade ,  Kotaro Gotanda ,  Atsushi Shinbo ,  Youichi Nakano ,  Hideo Kobayashi

IPC分类号： A61K31/5377 ,  C07D471/04 ,  C07D413/02 ,  A61K31/5025 ,  A61P9/10 ,  A61P13/10 ,  A61P13/12

CPC分类号： C07D487/04 ,  C07D487/14

摘要： The invention discloses quinoxaline derivatives or salts thereof having PDE9-inhibiting activity and being useful as treating agent of dysuria and the like, which are represented by the formula (I) in the formula, R1 and R2 each independently stands for hydrogen, halogen, alkyl, alkoxy, acyl, amino and the like, R3 stands for alkyl, aryl, saturated carbocyclic group, saturated heterocyclic group, acyl and the like, R4 stands for hydrogen, hydroxy, alkyl or amino, R5 and R8 each independently stands for hydrogen, halogen, alkyl, alkenyl, alkoxy, cyano or nitro, R6 and R7 each independently stands for hydrogen, halogen, alkyl, alkenyl, alkynyl, alkoxy, cyano, amino, carbocyclic group, heterocyclic group, COR9 or SO2R9, R9 stands for hydrogen, hydroxy, alkyl, amino, pyrrolidin-1-yl, piperidin-1-yl, pyperazin-1-yl or the like, X stands for S or O, and A1, A2 and A3 each independently stands for N or C.

摘要翻译： 本发明公开了具有PDE9抑制活性的喹喔啉衍生物或其盐，可用作式（I）所示的排尿困难等的治疗剂，R 1和R 2各自独立地表示氢，卤素，烷基 烷氧基，酰基，氨基等，R3代表烷基，芳基，饱和碳环基，饱和杂环基，酰基等，R4代表氢，羟基，烷基或氨基，R5和R8各自独立代表氢， 卤素，烷基，烯基，烷氧基，氰基或硝基，R6和R7各自独立地代表氢，卤素，烷基，烯基，炔基，烷氧基，氰基，氨基，碳环基，杂环基，COR9或SO2R9，R9代表氢， 羟基，烷基，氨基，吡咯烷-1-基，哌啶-1-基，哒嗪-1-基等，X表示S或O，并且，A1，A2和A3各自独立地表示N或C.

公开(公告)号：US08829000B2

公开(公告)日：2014-09-09

申请号：US13617683

申请日：2012-09-14

申请人： Makoto Okada ,  Shuichiro Sato ,  Kenji Kawade ,  Kotaro Gotanda ,  Atsushi Shinbo ,  Youichi Nakano ,  Hideo Kobayashi

发明人： Makoto Okada ,  Shuichiro Sato ,  Kenji Kawade ,  Kotaro Gotanda ,  Atsushi Shinbo ,  Youichi Nakano ,  Hideo Kobayashi

IPC分类号： A61K31/4985 ,  C07D487/04 ,  C07D487/14

CPC分类号： C07D487/04 ,  C07D487/14

摘要： The invention discloses quinoxaline derivatives or salts thereof having PDE9-inhibiting activity and being useful as treating agent of dysuria and the like, which are represented by the formula (I) in the formula, R1 and R2 each independently stands for hydrogen, halogen, alkyl, alkoxy, acyl, amino and the like, R3 stands for alkyl, aryl, saturated carbocyclic group, saturated heterocyclic group, acyl and the like, R4 stands for hydrogen, hydroxy, alkyl or amino, R5 and R8 each independently stands for hydrogen, halogen, alkyl, alkenyl, alkoxy, cyano or nitro, R6 and R7 each independently stands for hydrogen, halogen, alkyl, alkenyl, alkynyl, alkoxy, cyano, amino, carbocyclic group, heterocyclic group, COR9 or SO2R9, R9 stands for hydrogen, hydroxy, alkyl, amino, pyrrolidin-1-yl, piperidin-1-yl, pyperazin-1-yl or the like, X stands for S or O, and A1, A2 and A3 each independently stands for N or C.

摘要翻译： 本发明公开了具有PDE9抑制活性的喹喔啉衍生物或其盐，可用作式（I）所示的排尿困难等的治疗剂，R 1和R 2各自独立地表示氢，卤素，烷基 烷氧基，酰基，氨基等，R3代表烷基，芳基，饱和碳环基，饱和杂环基，酰基等，R4代表氢，羟基，烷基或氨基，R5和R8各自独立代表氢， 卤素，烷基，烯基，烷氧基，氰基或硝基，R6和R7各自独立地代表氢，卤素，烷基，烯基，炔基，烷氧基，氰基，氨基，碳环基，杂环基，COR9或SO2R9，R9代表氢， 羟基，烷基，氨基，吡咯烷-1-基，哌啶-1-基，哒嗪-1-基等，X表示S或O，并且，A1，A2和A3各自独立地表示N或C.